Table 4. Benzyl Analogues.
| compd no. | stereochem | R | T. b. brucei EC50 (μM)a | MRC-5 EC50 (μM)a | mouse microsomal intrinsic clearance (mL min–1 g–1) |
|---|---|---|---|---|---|
| 21 | R/S | phenyl | 0.22 | >15 | ND |
| 39 | R/S | 1-naphthyl | 50 | >50 | 28 |
| 40 | R/S | 4-chlorophenyl | 0.08 | >50 | 4.4 |
| 41 | R/S | 4-isopropylphenyl | 0.77 | >50 | 35 |
| 42 | R/S | 4-trifluoromethylphenyl | 0.11 | >50 | 3.0 |
| 43 | R/S | 4-fluorophenyl | 0.11 | >50 | 0.8 |
| 44 | R/S | 2,4-difluorophenyl | 2.3 | >50 | 0.5 |
| 45 | R | 4-chloro-3-fluorophenyl | 0.08 | >50 | 8.4 |
| 46 | R/S | 3,4-difluorophenyl | 0.11 | >50 | 1.9 |
| 47 | R | 4-fluorophenyl | 0.05 | >50 | 1.9 |
a
EC50 values are shown as mean values of two or more determinations. Standard deviation is typically within 2–3-fold from the EC50. ND = not determined.